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Last Updated: April 25, 2024

Claims for Patent: 9,186,414


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Summary for Patent: 9,186,414
Title:Composition for intraocular implantation of bevacizumab
Abstract: A solid, compressed pharmaceutical composition comprises i) a peptide active pharmaceutical ingredient, ii) a polysaccharide excipient and/or an albumin, and iii) an oligosaccharide excipient. The polysaccharide excipient may be hyaluronic acid, or the potassium salt thereof, and the oligosaccharide excipient may be trehalose.
Inventor(s): Khaw; Peng T. (London, GB), Brocchini; Stephen (London, GB), Khalili; Ashkan (Addison, IL)
Assignee: UCL Business PLC (London, GB)
Application Number:13/878,375
Patent Claims:1. A solid, compressed pharmaceutical composition comprising i) a peptide active pharmaceutical ingredient, ii) a polysaccharide excipient, and iii) an oligosaccharide excipient, wherein the polysaccharide excipient is present in the form of a potassium salt thereof.

2. A composition according to claim 1, wherein the oligosaccharide excipient is a non-reducing sugar.

3. A composition according to claim 1, wherein the oligosaccharide excipient is a disaccharide.

4. A composition according to claim 1, wherein the oligosaccharide excipient is trehalose.

5. A composition according to claim 1, wherein the polysaccharide excipient is non-sulphated.

6. A composition according to claim 1, wherein the polysaccharide excipient is a glycosaminoglycan.

7. A composition according to claim 6, wherein the polysaccharide excipient is hyaluronic acid.

8. A composition according to claim 1, wherein the composition contains one or more further, pharmaceutically acceptable excipients.

9. A composition according to claim 8, wherein the one or more further pharmaceutically acceptable excipients comprises an albumin.

10. A composition according to claim 1 wherein the composition contains potassium ions which are present as a potassium salt.

11. A composition according to claim 1, wherein the composition is sterile.

12. A composition according to claim 1, wherein the peptide active pharmaceutical ingredient, polysaccharide excipient, and oligosaccharide excipient are freeze dried, optionally in the presence of a potassium buffer salt.

13. A composition according to claim 12, wherein the peptide active pharmaceutical ingredient, polysaccharide excipient and oligosaccharide excipient are freeze dried together.

14. A composition according to claim 1, in the form of a tablet.

15. A composition according to claim 1, wherein the peptide active pharmaceutical ingredient has a molecular weight of around 0.5 kDa to around 250 kDa.

16. A composition according to claim 1, wherein the peptide active pharmaceutical ingredient is an antibody or an antigen-binding fragment thereof.

17. A composition according to claim 16, wherein the antibody is an anti-VEGF antibody.

18. A composition according to claim 1, wherein the composition is coated.

19. A composition according to claim 1, which is suitable for implantation.

20. A compressed pharmaceutical composition comprising a peptide active pharmaceutical ingredient, and potassium salt, wherein the potassium salt comprises the potassium salt of hyaluronic acid.

21. A composition according to claim 20, wherein the composition further comprises albumin.

22. A composition according to claim 1, containing one or more additional active pharmaceutical ingredients.

23. A method for the treatment or prevention of a condition selected from scarring, tumour growth and/or metastasis, vasculoproliferative conditions, conditions involving neovascularisation, vascular endothelial cell proliferation, angiogenesis, disorders of the eye selected from diabetic retinopathy, retinal vein occlusion, retinopathy of prematurity, age-related macular degeneration and choroidal neovascularisation, or for the treatment of a tumour that may be selected from brain tumour, breast tumour, kidney tumour, colorectal tumour, lung tumour, prostate tumour, head and neck tumours, stomach tumour, pancreatic tumour, skin tumour, cervical tumour, bone tumour, ovarian tumour, testicular tumour and liver tumours, the method comprising the implantation, into a suitable site of a subject in need of such treatment or prevention, of a composition according to claim 1.

24. A method for the treatment of neoplastic conditions, macular degeneration, diabetic retinopathy, or corneal angiogenesis, or for the prevention of scarring following glaucoma filtration surgery, the method comprising the implantation, into a suitable site of a subject in need of such treatment or prevention, of a composition according to claim 17.

25. A composition according to claim 17, wherein the antibody is bevacizumab.

26. A composition according to claim 10,wherein the potassium ions present as a potassium salt are present as a potassium buffer salt.

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